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Type II topoisomerase inhibitors

Anticancer drugsDrugHuman type II topoisomerasepyrimidinesTopo II


The invention relates to a new class of anticancer agents, able to inhibit the human enzyme topoisomerase II, thus reducing the proliferation of cancer cells. The new inhibitor compounds are to be used as treatment of various oncological pathologies, such as lung cancer or prostate cancer.

Technical features

The human type II topoisomerase (topo II) enzymes are essential for DNA modification. Different classes of topo II drugs have been developed in the last few decades but resistance to these drugs and serious side effects require the discovery of new safer topo II inhibitors for better anticancer therapies.

The proposed invention may be applied for the treatment of diseases and/or disorders associated to increased levels of expression or function of topo II, such as for example, various  neoplastic diseases, pre-malignant conditions (eg. hyperplasia, metaplasia or dysplasia), metastasis, benign tumors, hyperproliferative disorders.

Possible Applications

In the medical field, for the treatment of various neoplastic diseases (e.g. prostate cancer and lung cancer), either as an mono therapy, or in combination with radiotherapy or with other chemotherapeutics.


  • Excellent penetration of the cell membrane in a complex biological environment.